PURINONE COMPOUNDS AS KINASE INHIBITORS Russian patent published in 2018 - IPC C07D473/32 A61K31/52 A61K31/522 A61P35/00 A61P37/00 A61P35/02 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to novel compounds of formula (I), or a pharmaceutically acceptable salt thereof, or a stereoisomer having the properties of a Bruton (Btk) tyrosine kinase activity inhibitor. Compounds can be used to treat autoimmune diseases or conditions, heteroimmune diseases or conditions, including lymphoma, in the treatment of β-cell proliferative disorders, in the treatment of inflammatory diseases, such as asthma, inflammatory bowel disease, appendicitis, bronchitis, etc. In general formula (I)

L_a is -OCH₂-, -N(R₂₁)C(O)-, -C(O)N(R₂₁)- or -O-; Ar is a substituted or unsubstituted aryl, selected from phenyl, where the substituent can be selected from halogen, hydroxy, C₁-C₆alkoxy or C₁-C₆alkyl; R₃ is Y is a group selected from among C₃-C₆cycloalkyl, phenyl, optionally substituted C₁-C₄alkyl or C₁-C₄alkoxy; and bicyclic heteroaryl selected from a benzene ring fused to a 6-membered heterocycloalkyl comprising nitrogen and oxygen as heteroatoms; Z is C(=O) or N(R₂₁)C(=O); R₂₁ is H or unsubstituted C₁-C₆alkyl; R₂₄, is independently, unsubstituted C₁-C₄alkyl; n is 0 or 1; p is 0–2; R₆ is H or L-J-W; R₇ and R₈, independently, is H or L-J-W; L and J, is each independently a bond, or unsubstituted C₁-C₆alkylene; W is H, halogen, -CN or NR₂₅R₂₆; R₂₅ and R₂₆, is each independently H, unsubstituted C₁-C₆alkyl, unsubstituted C₃-C₆cycloalkyl, unsubstituted C₁-C₆heteroalkyl containing oxygen as a heteroatom, unsubstituted C₅-C₇heterocycloalkyl containing oxygen as a heteroatom, or substituted or unsubstituted C_3-C₁₂heteroaryl containing 1 to 2 nitrogen atoms as heteroatoms, where the substituent is selected from C₁-C₄alkyl.

EFFECT: invention has the properties of a Bruton tyrosine kinase activity inhibitor (Btk).

15 cl, 78 ex, 2 tbl